TWI801378B - 作為tnf活性調節劑之稠合五環咪唑衍生物 - Google Patents

作為tnf活性調節劑之稠合五環咪唑衍生物 Download PDF

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Publication number
TWI801378B
TWI801378B TW107113777A TW107113777A TWI801378B TW I801378 B TWI801378 B TW I801378B TW 107113777 A TW107113777 A TW 107113777A TW 107113777 A TW107113777 A TW 107113777A TW I801378 B TWI801378 B TW I801378B
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Taiwan
Prior art keywords
methyl
mmol
compound
difluoromethoxy
formula
Prior art date
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TW107113777A
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English (en)
Chinese (zh)
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TW201841918A (zh
Inventor
丹尼爾 克里斯多夫 布魯金斯
海羅 葛爾莎 泰瑞莎 迪
揚恩 佛瑞切
海倫 崔西 霍斯萊
馬丁 克里夫 亨琴斯
詹姆士 安德魯 強森
馬爾康 馬寇斯
宣孟陽
曉寧 徐
Original Assignee
比利時商Ucb生物製藥公司
法商賽諾菲公司
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=58632834&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI801378(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 比利時商Ucb生物製藥公司, 法商賽諾菲公司 filed Critical 比利時商Ucb生物製藥公司
Publication of TW201841918A publication Critical patent/TW201841918A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
TW107113777A 2017-04-25 2018-04-24 作為tnf活性調節劑之稠合五環咪唑衍生物 TWI801378B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
??17168027.5 2017-04-25
EP17168027 2017-04-25
EP17168027.5 2017-04-25

Publications (2)

Publication Number Publication Date
TW201841918A TW201841918A (zh) 2018-12-01
TWI801378B true TWI801378B (zh) 2023-05-11

Family

ID=58632834

Family Applications (1)

Application Number Title Priority Date Filing Date
TW107113777A TWI801378B (zh) 2017-04-25 2018-04-24 作為tnf活性調節劑之稠合五環咪唑衍生物

Country Status (33)

Country Link
US (4) US10980814B2 (fr)
EP (2) EP3939980B1 (fr)
JP (2) JP7083358B2 (fr)
KR (1) KR102565132B1 (fr)
CN (1) CN110582495B (fr)
AR (1) AR111426A1 (fr)
AU (1) AU2018259040B2 (fr)
CA (1) CA3058980A1 (fr)
CL (1) CL2019002875A1 (fr)
CO (1) CO2019012856A2 (fr)
CR (1) CR20190526A (fr)
DK (1) DK3615534T3 (fr)
EA (1) EA039049B1 (fr)
ES (2) ES2956555T3 (fr)
HR (1) HRP20211927T1 (fr)
HU (1) HUE056593T2 (fr)
IL (1) IL269890B (fr)
LT (1) LT3615534T (fr)
MA (2) MA49055B1 (fr)
MX (1) MX2019012443A (fr)
MY (1) MY197212A (fr)
PE (1) PE20200662A1 (fr)
PH (1) PH12019502182B1 (fr)
PL (2) PL3939980T3 (fr)
PT (2) PT3939980T (fr)
PY (1) PY1829804A (fr)
RS (1) RS62596B1 (fr)
SG (1) SG11201908871SA (fr)
SI (1) SI3615534T1 (fr)
TW (1) TWI801378B (fr)
UY (1) UY37700A (fr)
WO (1) WO2018197503A1 (fr)
ZA (1) ZA201906255B (fr)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201892144A1 (ru) * 2016-04-01 2019-04-30 Юсб Байофарма Спрл Конденсированные гексациклические производные имидазола в качестве модуляторов активности tnf
WO2018119142A1 (fr) 2016-12-21 2018-06-28 Amgen Inc. Formulations d'anticorps anti-tnf alpha
CA3117344A1 (fr) * 2018-10-24 2020-04-30 UCB Biopharma SRL Derives d'imidazole pentacycliques fusionnes utilises en tant que modulateurs de l'activite du tnf
AU2023385854A1 (en) 2022-11-23 2025-06-12 Forward Therapeutics, Inc. MODULATORS OF TNF-α ACTIVITY
AU2024264495A1 (en) 2023-04-26 2025-12-11 Sanofi Treating psoriasis using a small molecule inhibitor of tumor necrosis factor alpha
WO2024251282A1 (fr) * 2023-06-09 2024-12-12 上海翰森生物医药科技有限公司 Inhibiteur de dérivé pentacyclique, son procédé de préparation et son utilisation
TW202519231A (zh) 2023-07-04 2025-05-16 法商賽諾菲公司 結晶形式
WO2025038927A1 (fr) 2023-08-16 2025-02-20 Raythera, Inc. Modulateurs de l'activité du tnf alpha et leurs utilisations
WO2025068505A1 (fr) 2023-09-29 2025-04-03 Sanofi Préparation de dérivés d'imidazole pentacycliques pontés en tant que modulateurs de l'activité du tnf, intermédiaires et leur préparation
WO2025201449A1 (fr) * 2024-03-27 2025-10-02 海思科医药集团股份有限公司 Dérivés hétérocycliques et leur utilisation en médecine
WO2025212627A1 (fr) 2024-04-03 2025-10-09 Forward Therapeutics, Inc. Modulateurs de l'activité tnf-alpha
WO2025218735A1 (fr) * 2024-04-17 2025-10-23 上海翰森生物医药科技有限公司 Inhibiteur de dérivé pentacyclique, son procédé de préparation et son utilisation
WO2025247401A1 (fr) * 2024-05-31 2025-12-04 海思科医药集团股份有限公司 Dérivé hétérocyclique fusionné et son utilisation pharmaceutique
WO2025252251A1 (fr) * 2024-06-07 2025-12-11 上海翰森生物医药科技有限公司 Inhibiteur de dérivé hétérocyclique contenant de l'oxygène, son procédé de préparation et son utilisation
WO2026012303A1 (fr) * 2024-07-09 2026-01-15 Hangzhou Highlightll Pharmaceutical Co., Ltd NOUVEAUX COMPOSÉS BENZO[4,5]IMIDAZO EN TANT QUE MODULATEURS DE TNFα
WO2026022134A1 (fr) 2024-07-23 2026-01-29 Sanofi Nouveaux procédés d'aminocarbonylation
WO2026021586A1 (fr) * 2024-07-26 2026-01-29 上海瀚辰星泰医药科技有限公司 Composé polycyclique, son procédé de préparation et son utilisation
WO2026027449A1 (fr) 2024-07-29 2026-02-05 Sanofi Dérivés d'imidazole pentacycliques fusionnés
WO2026051930A1 (fr) * 2024-09-04 2026-03-12 苏州湃玥生物科技有限公司 Dérivé de benzimidazole pentacyclique fusionné utilisé en tant que modulateur d'activité de tnf, son procédé de préparation et son utilisation
WO2026055519A1 (fr) 2024-09-06 2026-03-12 Rapt Therapeutics, Inc. Composés imidazole à cycle fusionné
WO2026064602A1 (fr) * 2024-09-23 2026-03-26 Synnovation Therapeutics, Inc. COMPOSÉS HÉTÉROCYCLIQUES EN TANT QUE MODULATEURS DE L'ACTIVITÉ DU TNFα
WO2026068677A1 (fr) 2024-09-27 2026-04-02 Sanofi Procédés de préparation d'imidazoles pentacycliques fusionnés et d'intermédiaires

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016050975A1 (fr) * 2014-10-03 2016-04-07 Ucb Biopharma Sprl Dérivés d'imidazole pentacycliques fusionnés

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112014030940B1 (pt) 2012-06-11 2022-09-06 UCB Biopharma SRL Benzimidazóis que modulam tnf-alfa e composição farmacêutica compreendendo os mesmos
CN104619709B (zh) * 2012-07-13 2016-11-09 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
GB201212513D0 (en) * 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
GB201321728D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
AR104291A1 (es) 2015-04-17 2017-07-12 Abbvie Inc Moduladores tricíclicos de la señalización por tnf

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016050975A1 (fr) * 2014-10-03 2016-04-07 Ucb Biopharma Sprl Dérivés d'imidazole pentacycliques fusionnés

Also Published As

Publication number Publication date
US20210252012A1 (en) 2021-08-19
JP7299382B2 (ja) 2023-06-27
NZ758198A (en) 2024-01-26
JP2020517637A (ja) 2020-06-18
HRP20211927T1 (hr) 2022-03-18
CO2019012856A2 (es) 2020-01-17
BR112019020314A2 (pt) 2020-04-28
MX2019012443A (es) 2020-01-13
AU2018259040A1 (en) 2019-10-31
EP3615534B1 (fr) 2021-09-15
EP3939980B1 (fr) 2023-07-26
CN110582495A (zh) 2019-12-17
MY197212A (en) 2023-06-01
ES2956555T3 (es) 2023-12-22
PY1829804A (es) 2019-03-01
UY37700A (es) 2018-11-30
SG11201908871SA (en) 2019-10-30
MA49055B1 (fr) 2021-12-31
AU2018259040B2 (en) 2022-04-28
WO2018197503A1 (fr) 2018-11-01
LT3615534T (lt) 2021-11-25
JP2022116233A (ja) 2022-08-09
EP3615534A1 (fr) 2020-03-04
PH12019502182A1 (en) 2020-06-08
PL3615534T3 (pl) 2022-01-31
KR102565132B1 (ko) 2023-08-08
PL3939980T3 (pl) 2024-02-05
MA57699B1 (fr) 2023-11-30
US20230250105A1 (en) 2023-08-10
EP3939980A1 (fr) 2022-01-19
IL269890B (en) 2022-03-01
US20200046723A1 (en) 2020-02-13
EA201992407A1 (ru) 2020-04-06
ES2893807T3 (es) 2022-02-10
US10980814B2 (en) 2021-04-20
TW201841918A (zh) 2018-12-01
DK3615534T3 (da) 2021-10-18
RS62596B1 (sr) 2021-12-31
PT3939980T (pt) 2023-08-07
KR20190141200A (ko) 2019-12-23
JP7083358B2 (ja) 2022-06-10
CN110582495B (zh) 2022-04-01
PT3615534T (pt) 2021-10-21
CR20190526A (es) 2020-01-07
CA3058980A1 (fr) 2018-11-01
AR111426A1 (es) 2019-07-10
HUE056593T2 (hu) 2022-02-28
ZA201906255B (en) 2021-01-27
PE20200662A1 (es) 2020-06-11
MA49055A (fr) 2021-05-05
EA039049B1 (ru) 2021-11-26
SI3615534T1 (sl) 2022-01-31
CL2019002875A1 (es) 2020-03-06
PH12019502182B1 (en) 2024-01-31
US20250127795A1 (en) 2025-04-24

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